Company Name: |
Tianjin Kailiqi Biotechnology Co., Ltd.
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Tel: |
15076683720 |
Email: |
klq@cw-bio.com |
Products Intro: |
Product Name:DCH36-06 CAS:593273-05-3 Purity:≥98% Package:1g,5g,10g,25g根据客户需要分装 Remarks:Not For Human Use, Lab Use Only.
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Company Name: |
Bide Pharmatech Ltd.
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Tel: |
400-1647117 13681763483 |
Email: |
product02@bidepharm.com |
Products Intro: |
Product Name:1-(3-Chloro-4-methylphenyl)-5-(3-(furan-2-yl)allylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione CAS:593273-05-3 Purity:97% Package:100mg;250mg;1g Remarks:BD01395397
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| (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione Basic information |
Product Name: | (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione | Synonyms: | (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione;4,6(1H,5H)-Pyrimidinedione, 1-(3-chloro-4-methylphenyl)-5-[3-(2-furanyl)-2-propen-1-ylidene]dihydro-2-thioxo-;DCH36-06;(5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4;HATs,hypoacetylation,Apoptosis,DCH-36_06,inhibit,antiproliferative,p300,HAT,DCH36_06,Inhibitor,anti-tumor,CBP,Histone Acetyltransferase;1-(3-Chloro-4-methylphenyl)-5-(3-(furan-2-yl)allylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione | CAS: | 593273-05-3 | MF: | C18H13ClN2O3S | MW: | 372.83 | EINECS: | | Product Categories: | | Mol File: | 593273-05-3.mol | |
| (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione Chemical Properties |
storage temp. | 4°C, protect from light | solubility | DMSO : 125 mg/mL (335.27 mM; Need ultrasonic) | form | Solid | color | Orange to red |
| (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione Usage And Synthesis |
Biological Activity | DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity[1].
DCH36_06 (6.7-20 μM; 24-48 hours) treatment arrests cell cycle at G1 phase and induces apotosis in a dose-dependent manner in leukemic cells[1].DCH36_06 (5-10 μM; 24 hours) treatment significantly activates the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner[1].DCH36_06 shows potent antiproliferative activity against tested leukemia cell lines (CEM, MOLT3, MOLT4, Jurkat, MV4-11, THP-1, RS4; 11, KOPN8, Kasumi-1 and K562 cells) in a dose-dependent manner with IC50 values at single-digit micromolar range[1].
DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice[1]. | References | [1]. Wenchao Lu, et al. Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors. Bioorg Med Chem. 2018 Nov 1;26(20):5397-5407. |
| (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione Preparation Products And Raw materials |
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